丝裂原活化蛋白激酶激活的蛋白激酶2（MK2）抑制剂作为炎症性疾病的治疗方法
Inhibitors of Mitogen-Activated Protein Kinase-Activated Protein Kinase 2 (MK2) as Treatment for Inflammatory Diseases.
作者信息
Abdel-Magid Ahmed F
机构信息
PI Health Sciences, 100 Jade Park, Chelsea, Alabama 35043, United States.
出版信息
ACS Med Chem Lett. 2024 Aug 23;15(9):1421-1423. doi: 10.1021/acsmedchemlett.4c00393. eCollection 2024 Sep 12.
Abstract
The invention in this patent application relates to 9,10,11,12-tetrahydro-8-[1,4]diazepino[5',6':4,5]thieno[3,2-]quinolin-8-one derivatives represented herein generally by Formula . These compounds are inhibitors of MK2 kinases and may provide useful treatments for MK2-mediated diseases or disorders such as autoimmune disorders, chronic or acute inflammatory disorders, autoinflammatory disorders, fibrotic disorders, metabolic disorders, neoplasia, or cardiovascular or cerebrovascular disorders.
摘要
本专利申请中的发明涉及通式所示的9,10,11,12-四氢-8-[1,4]二氮杂卓并[5',6':4,5]噻吩并[3,2-]喹啉-8-酮衍生物。这些化合物是MK2激酶的抑制剂，可用于治疗MK2介导的疾病或病症，如自身免疫性疾病、慢性或急性炎症性疾病、自身炎症性疾病、纤维化疾病、代谢紊乱、肿瘤形成或心血管或脑血管疾病。
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ACR Open Rheumatol. 2023 Feb;5(2):63-70. doi: 10.1002/acr2.11517. Epub 2023 Jan 5.
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